Pitavastatin - Livalo Tablets- @- Cardiovascular (Aug 2009)
Drug Name:Pitavastatin - Livalo Tablets- @- Cardiovascular (Aug 2009)
List Of Brands:
Indication Type Description:
Drug Interaction
Indication
Adverse Reaction
Contra-Indications
Dosages/ Overdosage Etc
Patient Information
Pharmacology/ Pharmacokinetics
Pregnancy and lactation
Drug Interaction:
Erythromycin: Combination increases pitavastatin exposure.
Limit LIVALO to 1 mg once daily
.
Rifampin: Combination increases pitavastatin exposure.
Limit LIVALO to 2 mg once daily
.
Concomitant lipid-lowering therapies: Use with fibrates or lipid-modifying doses
(.1 g/day) of niacin increases the risk of adverse skeletal muscle effects.
Caution should be used when prescribing with LIVALO.
Indication:
Proprietary Name- Livalo tablets
Established Name - Pitavastatin - HMG- CoA reductase Inhibitor
Applicant- Kowa Research Institute Inc.
Indication-
Adjunct therapy to diet to reduce elevated cholesterol (Tc) , low density
Lipoprotein cholestrol (LDL-C), apoliprotein B ( Apo-B) , triglycerides(TG)
and to increase high-density lipoprotein cholesterol (HDL-C)
Dosage-
Greater than 4mg one daily
Approved by FDA on 3-8-2009 (Ref- FDA approved List- 2009)
Patent Expiry Date of drugs (Ref - IDMA Publication)
Chemical Category Manufacturer/ US Patent
Ingredient- Marketer Expiration Date
Pitavastatin Cardiovascular Nissan Chemical 05-01-2016
New Drugs Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
Pitavastatin 1mg/2mg 14-01-2005
tablet
Lipid Lowering agent
Adverse Reaction:
The most frequent adverse reactions (rate .2.0% in at least one marketed dose)
were myalgia, back pain, diarrhea, constipation and pain in extremity.
Contra-Indications:
CONTRAINDICATIONS.
Known hypersensitivity to product components
.
Active liver disease, which may include unexplained persistent elevations in hepatic
transaminase levels
.
Women who are pregnant or may become pregnant
.
Nursing mothers
.
Co-administration with cyclosporine
WARNINGS AND PRECAUTIONS
Skeletal muscle effects (e.g., myopathy and rhabdomyolysis):
Risks increase in a dose-dependent manner, with advanced age (.65),
renal impairment, and inadequately treated hypothyroidism.
Advise patients to promptly report unexplained and/or persistent muscle pain,
tenderness, or weakness, and discontinue LIVALO
.
Liver enzyme abnormalities: Persistent elevations in hepatic transaminases can occur.
Check liver enzyme tests before initiating therapy and as clinically indicated thereafter (5.2)
Dosages/ Overdosage Etc:
Indication-
Adjunct therapy to diet to reduce elevated cholesterol (Tc) , low density
Lipoprotein cholestrol (LDL-C), apoliprotein B ( Apo-B) , triglycerides(TG)
and to increase high-density lipoprotein cholesterol (HDL-C)
Dosage-
Greater than 4mg one daily
INDICATIONS AND USAGE
LIVALO is a HMG-CoA reductase inhibitor indicated for:
Patients with primary hyperlipidemia or mixed dyslipidemia as an adjunctive therapy
to diet to reduce elevated total cholesterol (TC), low-density lipoprotein
cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and
to increase high-density lipoprotein cholesterol (HDL-C)
Limitations of Use
Doses of LIVALO greater than 4 mg once daily were associated with an
increased risk for severe myopathy in premarketing clinical studies.
Do not exceed 4 mg once daily dosing of LIVALO.
The effect of LIVALO on cardiovascular morbidity and mortality has not
been determined.
LIVALO has not been studied in Fredrickson Type I, III, and V dyslipidemias.
DOSAGE AND ADMINISTRATION
LIVALO can be taken with or without food, at any time of day
Dose Range: 1 mg to 4 mg once daily
Primary hyperlipidemia and mixed dyslipidemia:
Starting dose 2 mg. When lowering of LDL-C is insufficient, the dosage may
be increased to a maximum of 4 mg per day.
Moderate and severe renal impairment (glomerular filtration rate
30, 59 and 15 -29 mL/min/1.73 m2, respectively) as well as end-stage renal disease
on hemodialysis:
Starting dose of 1 mg once daily and maximum dose of 2 mg once daily
DOSAGE FORMS AND STRENGTHS
Tablets: 1 mg, 2 mg, and 4 mg
Patient Information:
The patient should be informed of the following:
Dosing Time
LIVALO can be taken at any time of the day with or without food.
Muscle Pain
Patients should be advised to promptly notify their physician of any unexplained
muscle pain, tenderness, or weakness particularly if accompanied by malaise
or fever, or if these muscle signs or symptoms persist after discontinuing LIVALO.
They should discuss all medication, both prescription and over the counter, with their physician.
Pregnancy
Women of childbearing age should use an effective method of birth control to
prevent pregnancy while using LIVALO. Discuss future pregnancy plans
with your healthcare professional, and discuss when to stop LIVALO
if you are trying to conceive. If you are pregnant, stop taking LIVALO
and call your healthcare professional.
Breastfeeding
Women who are breastfeeding should not use LIVALO. If you have a lipid disorder
and are breastfeeding, stop taking LIVALO and consult with your healthcare professional.
Liver Enzymes
It is recommended that liver enzyme tests be checked before the initiation of LIVALO
and if signs or symptoms of liver injury occur. All patients treated with LIVALO
should be advised to report promptly any symptoms that may indicate
liver injury, including fatigue, anorexia, right upper abdominal discomfort,
dark urine or jaundice.
Pharmacology/ Pharmacokinetics:
Mechanism of Action
Pitavastatin competitively inhibits HMG-CoA reductase, which is a rate-determining
enzyme involved with biosynthesis of cholesterol, in a manner of competition
with the substrate so that it inhibits cholesterol synthesis in the liver.
As a result, the expression of LDL-receptors followed by the uptake of LDL
from blood to liver is accelerated and then the plasma TC decreases. Further,
the sustained inhibition of cholesterol synthesis in the liver decreases levels
of very low density lipoproteins.
Pharmacokinetics
Absorption: Pitavastatin peak plasma concentrations are achieved about
1 hour after oral administration.
Both Cmax and AUC0-inf increased in an approximately dose-proportional
manner for single LIVALO doses from 1 to 24 mg once daily.
The absolute bioavailability of pitavastatin oral solution is 51%.
Administration of LIVALO with a high fat meal (50% fat content) decreases
pitavastatin Cmax by 43% but does not significantly reduce pitavastatin AUC.
The Cmax and AUC of pitavastatin did not differ following evening or
morning drug administration. In healthy volunteers receiving 4 mg pitavastatin,
the percent change from baseline
Pregnancy and lactation:
Teratogenic effects: Pregnancy Category X
LIVALO is contraindicated in women who are or may become pregnant. Serum cholesterol
and TG increase during normal pregnancy, and cholesterol products are essential
for fetal development. Atherosclerosis is a chronic process and discontinuation of
lipid-lowering drugs during pregnancy should have little impact on long-term outcomes
of primary hyperlipidemia therapy [see Contraindications
There are no adequate and well
Nursing Mothers
It is not known whether pitavastatin is excreted in human milk, however, it has
been shown that a small amount of another drug in this class passes into human milk.
Rat studies have shown that pitavastatin is excreted into breast milk.
Because another drug in this class passes into human milk and HMG-CoA
reductase inhibitors have a potential to cause serious adverse reactions
in nursing infants, women who require LIVALO treatment should be advised
not to nurse their infants or to discontinue LIVALO [see Contraindications
Pediatric Use
Safety and effectiveness of LIVALO in pediatric patients have not been established.
Geriatric Use
Of the 2,800 patients randomized to LIVALO 1 mg to 4 mg in controlled clinical
studies, 1,209 (43%) were 65 years and older. No significant differences in efficacy
or safety were observed between elderly patients and younger patients.
However, greater sensitivity of some older individuals cannot be ruled out.
